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Alpha 1- and alpha 2-adrenoceptor selectivity of moxisylyte (thymoxamine) and its metabolites in the pithed rat.

Abstract
The selectivity of moxisylyte and its two metabolites deacetylmoxisylyte and demethyldeacetylmoxisylyte, for alpha 1- and alpha 2-adrenoceptors has been investigated in the pithed rat. Alpha 2-adrenoceptor blockade was measured by antagonism of the inhibitory effect of clonidine on the tachycardia produced by electrical stimulation of the cardiac accelerator nerves and of the pressor response to B-HT 933. alpha 1-Adrenoceptor blockade was measured by inhibition of the pressor response to (-)phenylephrine and to stimulation of the sympathetic outflow from the spinal cord. The three drugs (5 X 10(-6) to 2 X 10(-5) mol/kg i.v.) did not affect the inhibitory effect of clonidine and were equipotent as antagonists of the pressor response to B-HT 933, but only at the higher dose (10(-5) mol/kg). Moxisylyte and its metabolites (2.5 X 10(-6) to 10(-5) mol/kg i.v.) reduced the pressor response to (-)phenylephrine and to stimulation of the sympathetic outflow of the spinal cord in a dose-dependent manner. They were much more effective against (-)phenylephrine than B-HT 933. These results indicate that the three drugs are preferential alpha 1-adrenoceptor antagonists in vivo.
AuthorsJ Roquebert, A Malek, M H Creuzet, F Cognie, H Pontagnier
JournalArchives internationales de pharmacodynamie et de therapie (Arch Int Pharmacodyn Ther) Vol. 266 Issue 2 Pg. 282-93 (Dec 1983) ISSN: 0003-9780 [Print] Belgium
PMID6320755 (Publication Type: Journal Article)
Chemical References
  • Azepines
  • Receptors, Adrenergic, alpha
  • Phenylephrine
  • deacetylmoxisylyte
  • demethyldeacetylmoxisylyte
  • azepexole
  • Clonidine
  • Moxisylyte
Topics
  • Animals
  • Azepines (pharmacology)
  • Blood Pressure (drug effects)
  • Clonidine (pharmacology)
  • Electric Stimulation
  • Heart Rate (drug effects)
  • Male
  • Moxisylyte (analogs & derivatives, pharmacology)
  • Phenylephrine (pharmacology)
  • Rats
  • Rats, Inbred Strains
  • Receptors, Adrenergic, alpha (drug effects)
  • Spinal Cord (physiology)

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